4-Quinazolinamine, N-cyclohexyl-2-cyclopropyl-

Biological Activity

TH10785 is a DNA glycosylase 1 (OGG1) activator, TH10785 can interact with the phenylalanine-319 and glycine-42 amino acids of OGG1 and increase the enzyme activity, generates β, δ-lyase enzymatic function. TH10785 can control the catalytic activity mediated by a nitrogen base within its molecular structure. TH10785 can be used for the research of various diseases and aging connected with DNA oxidative lesions[1]. TH10785 (6.25 μM, 30 min) induces a de novo β, δ-elimination in vitro, allowing for AP sites as new substrates.TH10785 (10 μM, 0-2 min) allows OGG1 to increase DNA repair by addressing AP sites.TH10785 (0-20 μM, 72 h) induces OGG1 β, δ-lyase activity shifts cells toward PNKP1 dependence.TH10785 (2 μM) has affinity to OGG1 (KD=5.5 μM) increased when adding an AP site analog containing double-stranded DNA (KD=1.3 μM)[1].

storage

Store at -20°C

References

[1]. Maurice Michel, et al. Small-molecule activation of OGG1 increases oxidative DNA damage repair by gaining a new function. Science. 2022 Jun 24;376(6600):1471-1476.